americanpharmaceuticalreviewApril 27, 2017
Domain Therapeutics announced a collaboration agreement with Pfizer aimed at assessing the impact of mutations on different signaling pathways engaged by G protein-coupled receptors (GPCRs). Pfizer is interested in GPCRs with potential therapeutic relevance. Domain Therapeutics will use its proprietary bioSensAll technology to define signaling signatures for each of the wild-type and mutant receptors.
This collaboration aims to validate potential targets across a range of therapeutic indications by probing the structure-function relationships of various amino acid substitutions in each GPCR. Pfizer will utilize the results of specific mutations on intracellular signaling to guide further investigations in disease-specific models.
"We are very pleased to have signed this collaboration with Pfizer for the profiling of mutant GPCRs using the bioSensAll platform. It is yet another example of the wide applications of the technology, from target validation through to drug discovery and development," said Pascal Neuville, chief executive officer of Domain Therapeutics. "By building a better understanding of the signaling profile needed for efficacy, bioSensAll may reduce the attrition rate of early-stage drug development."
Domain Therapeutics will use bioSensAll to characterize the basal activities and signaling profile of known ligands of wild type receptors. It will then compare these profiles with those of mutant GPCRs. These differential signaling signatures will be used to inform target validation for different therapeutic indications.
GPCRs belong to the family of membrane receptors and constitute one of the main classes of therapeutic targets for many indications. The binding of a hormone or a specific ligand to a receptor’s binding site activates one or several pathways for intracellular signaling. This enables the cell to provide an adapted response to the change in its environment. The many drugs that target GPCRs represent about 40% of all treatments on the market, but only address 15% of GPCRs.
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